Small molecule inhibitors of G(alpha)i2 protein and uses thereof
AssigneesClark Atlanta University, Georgia Tech Research Corporation
InventorsShafiq A. Khan, Silvia Caggia, Adegboyega K. Oyelere, Subhasish Tapadar
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Abstract
The disclosure relates to novel compounds and methods of use of the compounds to maintain the Gαi2 protein in its inactive GDP-bound state. The disclosure describes the knockdown or inhibition of Gαi2 negatively regulated migration of breast and ovarian cancer cell lines. The novel compounds inhibit the migratory behavior of PC3, DU145 and E006AA prostate cancer cell lines. Specifically, the novel compounds block the activation of Gαi2 in oxytocin-stimulated prostate cancer PC3 cells and inhibits the migratory capability of DU145 cells overexpressing constitutively active form of Gαi2, under basal and EGF-stimulated conditions.
Claims6
A compound having the following structure:
A compound having the following structure:
A compound having the following structure:
A method of treating cancer, comprising administering to a subject in need thereof a compound of Formula I or Formula II:
- wherein,
- R1, R2 and R3 are each independently selected from the group consisting of H, OH and halogen;
- R4 is selected from the group consisting of H, alkyl, halo-alkyl, aryl, and pyridyl, wherein the aryl and pyridyl groups are optionally substituted at the ortho, meta and para positions;
- R5 is selected from the group consisting of H, methyl and ethyl;
- R6 is selected from the group consisting of H, OH and halogen;
- and
- R7 is OH or OMe;
- wherein,
- R1a, R2a and R3a are each independently selected from the group consisting of H, OH and halogen;
- R4a is selected from the group consisting of H, alkyl, halo-alkyl, aryl and pyridyl, wherein the phenyl and pyridyl are optionally substituted at the ortho, meta and para positions;
- R5a is selected from the group consisting of H, methyl and ethyl;
- R6a is H or halogen;
- R7a is OH or OMe;
- and,
- X is S or O;
- to inhibit cell migration in prostate cancer, breast cancer, or ovarian cancer.
A method of treating cancer, comprising administering to a subject in need thereof a compound having the structure:
- to inhibit cell migration in prostate cancer, breast cancer, or ovarian cancer.
Dependencies are inferred from the claim text.